Elestat

"Plants produce round pollen grains. Individual grains are too tiny to see with the naked eye, but some can form large, visible clusters. For fertilization to take place and seeds to form in some plants, pollen must be moved from the flower of one"...

Elestat

WARNINGS

Included as part of the PRECAUTIONS section.

PRECAUTIONS

Contamination of Tip and Solution

Patients should be instructed to avoid allowing the tip of the dispensing container
to contact the eye, surrounding structures, fingers, or any other surface in
order to avoid contamination of the solution by common bacteria known to cause
ocular infections. Serious damage to the eye and subsequent loss of vision may
result from using contaminated solutions.

Bottle should be kept tightly closed when not in use.

Use with Contact Lenses

Patients should be advised not to wear a contact lens if their eye is red.
ELESTAT® ophthalmic solution should not be used to treat contact
lens-related irritation.

The preservative in ELESTAT®, benzalkonium chloride, may be absorbed
by soft contact lenses. Contact lenses should be removed prior to instillation
of ELESTAT® ophthalmic solution and may be reinserted after 10 minutes
following its administration.

Topical Ophthalmic Use Only

ELESTAT® is for topical ophthalmic use only and not for injection
or oral use.

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

In 18-month or 2-year dietary carcinogenicity studies in mice or rats, respectively,
epinastine was not carcinogenic at doses up to 40 mg/kg [approximately 30,000
times higher than the MROHD, assuming 100% absorption in humans and animals].

Epinastine in newly synthesized batches was negative for mutagenicity in the
Ames/Salmonella assay and in vitro chromosome aberration assay using
human lymphocytes. Positive results were seen with early batches of epinastine
in two in vitro chromosomal aberration studies conducted in 1980s with
human peripheral lymphocytes and with V79 cells, respectively. Epinastine was
negative in the in vivo clastogenicity studies, including the mouse micronucleus
assay and chromosome aberration assay in Chinese hamsters. Epinastine was also
negative in the cell transformation assay using Syrian hamster embryo cells,
V79/HGPRT mammalian cell point mutation assay, and in vivo/in vitro unscheduled
DNA synthesis assay using rat primary hepatocytes.

Epinastine had no effect on fertility of male rats. Decreased fertility in
female rats was observed at an oral dose up to approximately 90,000 times the
MROHD.

Use In Specific Populations

Pregnancy

Teratogenic Effects - Pregnancy Category C

In an embryofetal developmental study in pregnant rats, maternal toxicity with
no embryofetal effects was observed at an oral dose that was approximately 150,000
times the maximum recommended ocular human dose (MROHD) of 0.0014 mg/kg/day
on a mg/kg basis. Total resorptions and abortion were observed in an embryofetal
study in pregnant rabbits at an oral dose that was approximately 55,000 times
the MROHD. In both studies, no drug-induced teratogenic effects were noted.

Epinastine reduced pup body weight gain following an oral dose to pregnant
rats that was approximately 90,000 times the MROHD.

There are, however, no adequate and well-controlled studies in pregnant women.
Because animal reproduction studies are not always predictive of human response,
ELESTAT® ophthalmic solution should be used during pregnancy only
if the potential benefit justifies the potential risk to the fetus.

Nursing Mothers

A study in lactating rats revealed excretion of epinastine in the breast milk.
It is not known whether this drug is excreted in human milk. Because many drugs
are excreted in human milk, caution should be exercised when ELESTAT®
ophthalmic solution is administered to a nursing woman.

Pediatric Use

Safety and effectiveness in pediatric patients below the age of 2 years have
not been established.

Geriatric Use

No overall differences in safety or effectiveness have been observed between
elderly and younger patients.

Last reviewed on RxList: 1/9/2012
This monograph has been modified to include the generic and brand name in many instances.